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Enzastaurin
- LY 317615
- Soluble in DMSO
- MF: C32H29N5O2
- MW: 515.6
Description
Enzastaurin is a selective protein kinase C β (PKCβ) inhibitor that also inhibits PKCα, PKCγ and PKCε with IC50 values of 39, 83 and 110 nM, respectively.
PKC signaling regulates proliferation, survival, angiogenesis and vascular responses. Enzastaurin is useful for evaluating PKCβ-dependent signaling and downstream pathway effects in oncology and vascular biology models.
Key Features
- Selective PKCβ-targeted kinase inhibitor
- IC50: 6 nM for PKCβ
- Also inhibits PKCα, PKCγ and PKCε at higher concentrations
- Modulates PKC-dependent survival and angiogenic signaling
Applications
- PKC signaling research
- Cancer cell proliferation and survival assays
- Angiogenesis pathway studies
- Kinase selectivity and pathway crosstalk profiling
More Information
| Parent CAS No. | 170364-57-5 |
|---|---|
| Chemical Name | 3-(1-methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione |
| SMILES | C1(C2=CN(C)C3C=CC=CC2=3)C(=O)NC(=O)C=1C1C2C=CC=CC=2N(C2CCN(CC3C=CC=CN=3)CC2)C=1 |
| MFCD | MFCD11840851 |
| InChi | InChI=1S/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39) |
| InChiKey | AXRCEOKUDYDWLF-UHFFFAOYSA-N |
| CID | 176167 |
| Short Description | PKC-β inhibitor |
References
- JR Graff et al. The Protein Kinase Cβ–Selective Inhibitor, Enzastaurin (LY317615.HCl), Suppresses Signaling through the AKT Pathway, Induces Apoptosis, and Suppresses Growth of Human Colon Cancer (...). Cancer Res. 2005, 65, 7462-7469.
- MA Rizvi et al. Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines. Mol. Cancer Ther. 2006, 5, 1783-1789.
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